Assay Detail
Binding
CHEMBL5336739
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Activation of GST-tagged FXR LBD (unknown origin) using biotinylated Src-1 peptide as substrate by AlphaScreen assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Chemical exploration of TGR5 functional hot-spots: Synthesis and structure-activity relationships of C7- and C23-Substituted cholic acid derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 25 | 4.50 | 5.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5409189 | — | — | 1 | 5.52 |
| CHEMBL5420121 | — | — | 1 | 4.66 |
| CHEMBL5436516 | — | — | 1 | 4.63 |
| CHEMBL5396857 | — | — | 1 | 4.57 |
| CHEMBL5408411 | — | — | 1 | 4.46 |
| CHEMBL5433595 | — | — | 1 | 4.36 |
| CHEMBL5437734 | — | — | 1 | 4.28 |
| CHEMBL5425544 | — | — | 1 | 4.26 |
| CHEMBL205596 | CHOLIC ACID | 4.0 | 1 | 4.14 |
| CHEMBL5438844 | — | — | 1 | 4.12 |
| CHEMBL567640 | — | — | 1 | - |
| CHEMBL5430282 | — | — | 1 | - |
| CHEMBL5435161 | — | — | 1 | - |
| CHEMBL5411038 | — | — | 1 | - |
| CHEMBL5424602 | — | — | 1 | - |
| CHEMBL5412957 | — | — | 1 | - |
| CHEMBL5440980 | — | — | 1 | - |
| CHEMBL5431752 | — | — | 1 | - |
| CHEMBL5418782 | — | — | 1 | - |
| CHEMBL5407394 | — | — | 1 | - |
| CHEMBL5416586 | — | — | 1 | - |
| CHEMBL5431182 | — | — | 1 | - |
| CHEMBL5422960 | — | — | 1 | - |
| CHEMBL5426065 | — | — | 1 | - |
| CHEMBL5424633 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5409189 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5420121 | — | EC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL5436516 | — | EC50 | = | 23500.0 | nM | 4.63 |
| CHEMBL5396857 | — | EC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL5408411 | — | EC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL5433595 | — | EC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL5437734 | — | EC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL5425544 | — | EC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL205596 | CHOLIC ACID | EC50 | = | 73000.0 | nM | 4.14 |
| CHEMBL5438844 | — | EC50 | = | 76500.0 | nM | 4.12 |
| CHEMBL567640 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5430282 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5435161 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5411038 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5424602 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5412957 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5440980 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5431752 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5418782 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5407394 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5416586 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5431182 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5422960 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5426065 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5424633 | — | EC50 | > | 100000.0 | nM | - |